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1 2009

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Synthesis, Pharmacological Properties, and Computational Study of 1-[3-(4-Aryl-1-piperazinyl)]propyl Derivatives of Amides of 7 Methyl-3-phenyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-5-carboxylic Acid

Sabiniarz A., Śladowska H., Sapa J., Filipek B., Dudek M., Godyń G., Żyta J.

Polish Journal of Chemistry

2009

Vol. 83, nr 5

981-998

Two series of novel 1-[3-(4-aryl-1-piperazinyl)]- and 1-[2-hydroxy-3-(4-aryl-1- piperazinyl)]propyl derivatives of amides of 7-methyl-3-phenyl-2,4-dioxo- 1,2,3,4- tetrahydro - pyrido[2,3-d]pyrimidine-5-carboxylic acid (32–46) were synthesized. In the ”writhing syndrome” test all the amides studied displayed an algesic action. The most potent effect was produced by compounds 32, 34, and 46. In the ”hot plate” test only two amides, 34 and 37, showed strong an algesic activity. Further more, most of the investigated substances significantly suppressed spontaneous locomotor activity in mice and prolonged barbiturate sleep of these animals. QSAR analysis of the 14 new and 14 earlier described compounds was made.